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A series of new orthogonally protected α‐CF3‐substituted α‐amino carboxylates, and α‐amino phosphonates decorated with pharmacophore isoquinolone core has been elaborated through the Rh(III)‐catalyzed C−H activation/annulation of aryl hydroxamates with propargyl‐containing α‐amino acid derivatives and their phosphorus analogues. [ABSTRACT FROM AUTHOR]

An efficient method for the CF3-carbenoid C-7 functionalization of N-pyrimidylindolines has been developed. This protocol uses readily available methyl 3,3,3-trifluoro-2-diazopropionate as a cross-coupling partner and smoothly proceeds under chelation-controlled RhIII catalysis. The reactions provide the indoline products with high regioselectivity within a few hours and allow for the introduction of both the CF3 and carboxylate functions at the C-7 position. [ABSTRACT FROM AUTHOR]

An efficient method for the CF3-carbenoid C-H functionalization of benzenes and indoles using readily available methyl 3,3,3-trifluoro-2-diazopropionate as a cross-coupling partner under chelation-controlled RhIII catalysis has been developed. The reactions proceeded smoothly with high regioselectivity in a few hours and allowed the simultaneous introduction of CF3 and carboxylate functions into the 2-position of directing-group-containing benzenes and indoles. [ABSTRACT FROM AUTHOR]